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Beilstein J. Org. Chem. 2024, 20, 950–958, doi:10.3762/bjoc.20.85
Graphical Abstract
Figure 1: Tetrazole drugs, current assembly strategies, and novel building block strategy.
Scheme 1: Synthesis of tetrazole building blocks. Isolated yields.
Scheme 2: Substrate scope of Passerini products 3. Isolated yields.
Scheme 3: Substrate scope of Ugi products 4 and 5. Isolated yields.
Scheme 4: Synthesis of tetrazole building block 6. Isolated yield.
Beilstein J. Org. Chem. 2019, 15, 513–520, doi:10.3762/bjoc.15.45
Scheme 1: MCR approach to indole-based macrocycles; a more effective strategy is proposed in this work, based...
Scheme 2: Reaction of unprotected diamines 3 with cyclic anhydrides 4 at rt affording α,ω-amino acids 5 in qu...
Scheme 3: Ugi macrocyclization in a one-pot fashion and synthesis of diverse indole-based macrocycles. The ci...
Figure 1: (A) Modeling of the macrocycle 2h (cyan sticks) and 2n (magenta sticks) into the MDM2 receptor (PDB...
Figure 2: (A) Overlay of 1 H,15N-HSQC spectra of the reference MDM2 (red) and the titration steps with the 2i...